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公开(公告)号:US4136116A
公开(公告)日:1979-01-23
申请号:US558609
申请日:1975-03-14
申请人: Emilio Kyburz , Hans Spiegelberg
发明人: Emilio Kyburz , Hans Spiegelberg
IPC分类号: C07C13/547 , C07C63/331 , C07C65/38
CPC分类号: C07C65/38 , C07C13/547 , C07C63/331 , C07C2103/32
摘要: 1-Methyl(or acetyl)-5H-dibenzo[a,d]cycloheptenes and 1-methyl(or acetyl)-10,11-dihydro-5H-dibenzo[a,d]cycloheptenes bearing a basic side chain at the 5-position, such as a 3-mono- or dimethylaminopropylidene, a 3-mono- or dimethylaminopropyl or a 3-dimethylaminopropylidene(or propyl)-N-oxide, intermediates and processes for their preparation, are described. The end products are useful antidepressants.
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公开(公告)号:US4749791A
公开(公告)日:1988-06-07
申请号:US121987
申请日:1987-11-18
申请人: Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
发明人: Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
IPC分类号: A61K31/395 , A61P25/28 , C07D221/10 , C07D225/06 , C07D221/06
CPC分类号: C07D221/10 , C07D225/06
摘要: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen,as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
摘要翻译: 苯甲酸甲酯,其中R1和R2独立地是氢或氯,R3是氢,氟,氯,溴或甲氧基,R4是氢,氯或甲氧基,R5是氢,乙酰基,丙酰基,苯甲酰基,氯代苯甲酰基, 甲氧基苯甲酰基或苯乙酰基,条件是R 1至R 4基团中的2或3个为氢,以及许多相应的苯并[f]喹啉可以通过氧化制备这些苯并吖嗪酮,适于控制或预防脑部 不足或用于改善哺乳动物的认知功能。 它们可以根据各种方法制备并且可以制备成药物组合物。
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公开(公告)号:US4732979A
公开(公告)日:1988-03-22
申请号:US5712
申请日:1987-01-21
申请人: Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
发明人: Werner Aschwanden , Rene Imhof , Roland Jakob , Emilio Kyburz
IPC分类号: A61K31/395 , A61P25/28 , C07D221/10 , C07D225/06 , C07D227/08 , C07D221/06
CPC分类号: C07D221/10 , C07D225/06
摘要: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
摘要翻译: 苯甲酸甲酯,其中R1和R2独立地是氢或氯,R3是氢,氟,氯,溴或甲氧基,R4是氢,氯或甲氧基,R5是氢,乙酰基,丙酰基,苯甲酰基,氯代苯甲酰基, 甲氧基苯甲酰基或苯乙酰基,条件是R 1至R 4基团中的2或3个为氢。 以及可以通过氧化制备这些苯并吖嗪酮的许多相应的苯并[f]喹啉适用于控制或预防脑功能不全或改善哺乳动物的认知功能。 它们可以根据各种方法制备并且可以制备成药物组合物。
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公开(公告)号:US4616010A
公开(公告)日:1986-10-07
申请号:US831206
申请日:1986-02-20
申请人: Walter Hunkeler , Emilio Kyburz
发明人: Walter Hunkeler , Emilio Kyburz
IPC分类号: A61K31/55 , A61P25/20 , C07D243/00 , C07D333/00 , C07D487/14 , C07D495/22 , C07D513/22
CPC分类号: C07D487/14
摘要: Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma., and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.
摘要翻译: 作为下式的咪唑并二氮杂衍生物的化合物,其中A与由α和β表示的碳原子一起表示R1和R2之一,R2表示氢,另一个表示氢,卤素或三氟甲基,R3和R4 各自表示氢或卤素,n表示数字2或3,已经发现了以γ表示的具有(S) - 或(R,S) - 构型的化合物及其药学上可接受的酸加成盐 其具有抗焦虑,抗惊厥,肌肉松弛剂和镇静催眠特性。 它们可以使用合适的惰性载体制备成组合物,包括药学上可接受的组合物。
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公开(公告)号:US4461906A
公开(公告)日:1984-07-24
申请号:US172607
申请日:1980-07-28
申请人: Werner Aschwanden , Emilio Kyburz
发明人: Werner Aschwanden , Emilio Kyburz
IPC分类号: C07D207/27 , A61K31/40 , C07D207/26 , C07D207/263 , C07D207/273 , C07F7/10 , C07F7/18 , C07D407/12
CPC分类号: C07D207/27 , C07D207/273 , C07F7/10 , C07F7/1856 , Y10S514/878
摘要: 1-Substituted-2-pyrrolidinones of the formula ##STR1## wherein one of R.sup.1, R.sup.2 and R.sup.3 represents hydroxy and the remaining substituents represent hydrogen,are capable of counteracting cerebral insufficiency produced experimentally in animal tests. They can be used therapeutically in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. They can be manufactured from novel intermediates and can be processed to provide medicaments.
摘要翻译: 1-取代的2-吡咯烷酮,其中R 1,R 2和R 3中的一个代表羟基,其余的取代基代表氢,能够抵抗动物实验中实验产生的脑功能不全。 它们可用于治疗或预防脑功能不全或提高智力能力。 它们可以由新型中间体制成,可以加工成药物。
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公开(公告)号:US4386028A
公开(公告)日:1983-05-31
申请号:US403947
申请日:1982-07-30
申请人: Walter Hunkeler , Emilio Kyburz
发明人: Walter Hunkeler , Emilio Kyburz
IPC分类号: C07D495/22 , A61K31/55 , A61K31/551 , A61P25/20 , A61P33/10 , A61P39/02 , A61P43/00 , C07D243/14 , C07D265/26 , C07D471/22 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07F9/6561
CPC分类号: C07D265/26 , A61K31/55 , C07D243/14 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/906
摘要: There is provided imidazodiazepines of the formula ##STR1## wherein R.sup.1 is methyl, ethyl or isopropyl, one of R.sup.4 and R.sup.5 is hydrogen and the other is nitro or cyano, and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene and the carbon atom denoted as .gamma. has the (S)- or (R,S)-configuration, and X is an oxygen or sulphur atom,and their pharmaceutically acceptable acid addition salts. The compounds are useful in the antagonization of the central-depressant muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines. Also provided are methods for making the compounds.
摘要翻译: 提供下式的咪唑并二氮杂其中R 1是甲基,乙基或异丙基,R 4和R 5之一是氢,另一个是硝基或氰基,R 2是氢,R 3是氢或低级烷基或R 2, R3一起是二亚甲基,三亚甲基或亚丙烯基,并且表示为γ的碳原子具有(S) - 或(R,S) - 构型,X是氧或硫原子,以及它们的药学上可接受的酸加成盐。 该化合物可用于拮抗具有镇静作用的1,4-苯二氮卓类的中枢抑制肌肉松弛剂,共济失调,降血压和呼吸抑制剂性质。 它们还可以用于抑制其他指征领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性,例如血吸虫病活性的1,4-苯并二氮杂。 还提供了制备化合物的方法。
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公开(公告)号:US4363762A
公开(公告)日:1982-12-14
申请号:US322091
申请日:1981-11-16
申请人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号: A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号: C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要: Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of: ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonising the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillising activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillising participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译: 其中A与表示为α和β的两个碳原子一起选自下列组成的组:虚线表示组(a)和(b)中存在的双键, ,D为> C = O或> C = S,R 1选自氰基,低级烷酰基和式-COOR 4基团,R 4选自甲基,乙基,异丙基和2- 羟乙基,R 5选自氢,三氟甲基和卤素,R 6选自氢,三氟甲基,卤素和低级烷基,R 2是氢,R 3是氢或低级烷基或R 2和R 3一起是 三亚甲基或亚丙烯基,并且表示为γ的碳原子具有S-或R,S-构型及其药学上可接受的盐,并且可用于拮抗中枢抑制剂,肌肉松弛剂,共济失调,降血压和呼吸 具有镇静作用的1,4-苯并二氮杂的抑制剂性质。 例如,可以使用它们作为解毒剂,在中毒的情况下,过量摄入具有镇定作用的1,4-苯二氮卓类药物参与,或用于缩短由该1,4-苯并二氮杂卓诱导的麻醉。 它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性,例如血吸虫半衰期活性1,4-苯并二氮杂如(+) - 5-(邻 - 氯苯基) )-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。 还提出了产生咪唑并氮杂衍生物的方法及其中间体。
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公开(公告)号:US4346036A
公开(公告)日:1982-08-24
申请号:US322113
申请日:1981-11-16
申请人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号: A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号: C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要: Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration,and pharmaceutically acceptable salts thereof are presented and have utility for antagonising the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译: 其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式(a)和(b)中存在的双键: D是> C = O或> C = S,R 1选自氰基,低级烷酰基和式-COOR 4基团,R 4选自甲基,乙基,异丙基和2-羟基乙基 R5选自氢,三氟甲基和卤素,R6选自氢,三氟甲基,卤素和低级烷基,R2是氢,R3是氢或低级烷基或R2和R3一起是三亚甲基 或丙烯并且表示为γ的碳原子具有S-或R,S-构型及其药学上可接受的盐,并且具有拮抗中枢抑制剂,肌肉松弛剂,共济失调,降血压和呼吸的效用 具有镇静作用的1,4-苯并二氮杂类的抑制剂性质。 例如,可以使用它们作为解毒剂,在中毒的情况下,过量摄入具有镇静作用的1,4-苯二氮卓类药物参与,或用于缩短由1,4-苯并二氮杂卓诱导的麻醉。 它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性,例如血吸虫半衰期活性1,4-苯并二氮杂如(+) - 5-(邻 - 氯苯基) )-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。 还提出了产生咪唑并氮杂衍生物的方法及其中间体。
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公开(公告)号:US4346034A
公开(公告)日:1982-08-24
申请号:US321941
申请日:1981-11-16
申请人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号: A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号: C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要: Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is
摘要翻译: 其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式(a)和(b)中存在的双键: D是
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公开(公告)号:US4346033A
公开(公告)日:1982-08-24
申请号:US321821
申请日:1981-11-16
申请人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
发明人: Max Gerecke , Willy Haefely , Walter Hunkeler , Emilio Kyburz , Hanns Mohler , Lorenzo Pieri , Petar Polc
IPC分类号: A61K31/55 , A61K31/551 , A61P33/10 , A61P39/02 , C07D243/14 , C07D243/16 , C07D243/18 , C07D243/24 , C07D265/26 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , C07D495/22 , C07D498/04 , C07D513/14
CPC分类号: C07D265/26 , C07D243/14 , C07D333/42 , C07D487/04 , C07D487/14 , C07D495/04 , C07D495/14 , Y10S514/823 , Y10S514/906 , Y10S514/929 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要: Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is selected from the group consisting of ##STR2## the dotted line represents the double bond present in groups (a) and (b), D is >C.dbd.O or >C.dbd.S, R.sup.1 is selected from the group consisting of cyano, lower alkanoyl and a group of the formula --COOR.sup.4, R.sup.4 is selected from the group consisting of methyl, ethyl, isopropyl and 2-hydroxyethyl, R.sup.5 is selected from the group consisting of hydrogen, trifluoromethyl and halogen and R.sup.6 is selected from the group consisting of hydrogen, trifluoromethyl, halogen and lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together are trimethylene or propenylene and the carbon atom denoted as .gamma. has the S- or R,S-configuration, and pharmaceutically acceptable salts thereof are presented and have utility for antagonizing the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity. They can be used, for example, as antidotes in the case of intoxications in which excessive intake of 1,4-benzodiazepines which have tranquillizing participates, or for shortening an anaesthesia induced by such 1,4-benzodiazepines. They can also be used for suppressing the activities on the central nervous system of 1,4-benzodiazepines used in other fields of indication, for example of schistosomicidally-active 1,4-benzodiazepines such as (+)-5-(o-chlorophenyl)-1,3-dihydro-3-methyl-7-nitro-2H-1,4-benzodiazepin-2-one.Also presented are processes to produce the imidazodiazepine derivatives and intermediates therefor.
摘要翻译: 其中A与表示为α和β的两个碳原子一起选自由下列组成的组的虚线表示式(a)和(b)中存在的双键: D是> C = O或> C = S,R 1选自氰基,低级烷酰基和式-COOR 4基团,R 4选自甲基,乙基,异丙基和2-羟基乙基 R5选自氢,三氟甲基和卤素,R6选自氢,三氟甲基,卤素和低级烷基,R2是氢,R3是氢或低级烷基或R2和R3一起是三亚甲基 或丙烯并且表示为γ的碳原子具有S-或R,S-构型及其药学上可接受的盐,并且具有拮抗中枢抑制剂,肌肉松弛剂,共济失调,降血压和呼吸的效用 具有镇静作用的1,4-苯并二氮杂类的抑制剂性质。 例如,可以使用它们作为解毒剂,在中毒的情况下,过量摄入具有镇静作用的1,4-苯二氮卓类药物参与,或用于缩短由1,4-苯并二氮杂卓诱导的麻醉。 它们还可用于抑制其他适应症领域中使用的1,4-苯并二氮杂类的中枢神经系统的活性,例如血吸虫半衰期活性1,4-苯并二氮杂如(+) - 5-(邻 - 氯苯基) )-1,3-二氢-3-甲基-7-硝基-2H-1,4-苯并二氮杂-2-酮。 还提出了产生咪唑并氮杂衍生物的方法及其中间体。
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